competitive

4-Diethylaminobenzaldehyde, a reversible aldehyde dehydrogenase (ALDH) inhibitor (Ki: 4 nM for ALDH1), exhibits a potent anti-androgenic effect (IC50: 1.71 μM).

Sulbactam sodium (CP-45899-2) (Unasyn) is an irreversible β-lactamase inhibitor.

Nikkomycin Z (Nikkomycin Z from Streptomyces tendae) is a competitive chitin synthase inhibitor.It inhibitor of the growth of filamentous fungi, insects, acarids and yeasts.

Obtusin is a natural product.

Sulbactam (CP45899) is a semi-synthetic beta-lactamase inhibitor. The beta-lactam ring of sulbactam irreversibly binds to beta-lactamase at or near its active site, thereby blocking enzyme activity and preventing metabolism of other beta-lactam antibiotics by the enzyme. Combining this agent with a beta-lactamase susceptible antibiotic, such as penicillins or a cephalosporin, to treat infections caused by beta-lactamase producing organisms, results in a decreased turnover rate of the beta-lactamase sensitive antibiotic and enhances its antibacterial activity.

Bicuculline is an alkaloid extracted from Corydalis decumbens, acting as a competitive antagonist of the neurotransmitter GABAA receptor (IC50 = 2 μM). It also blocks Ca2+-activated potassium (SK) channels and inhibits slow afterhyperpolarization (slow AHP). Bicuculline has anticonvulsant effects and is commonly used to establish mouse seizure models.

NU2058 (O(6)-Cyclohexylmethylguanine) is a guanine-based CDK inhibitor, also inhibits DNA topoisomerase II ATPase activity.

DNQX (FG 9041) is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.5 and 0.1 μM for AMPA and kainate receptors, respectively)

PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 µM)

Osthenol is a natural product, and is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM).It shows antitumor-promoting activity, it also has antifungal and antibacterial activities.

U0126-etoh (U0126 Ethanol) is a non-ATP competitive inhibitor of MEK1 (IC50=72 nM) and MEK2 (IC50=58 nM) with selectivity. U0126-EtOH inhibited autophagy and mitophagy.

Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Adezmapimod (SB 203580) is a selective, ATP-competitive p38 MAPK inhibitor (IC50=0.3-0.5 μM) that activates autophagy and mitochondrial autophagy, with more than 100-fold higher selectivity over PKB, LCK, and GSK-3β.

Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.

AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.

Y-27632 is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.

Semaglutide Acetate is a GLP-1R agonist (EC50=6.2 pM) with long-acting, selective, competitive, and oral efficacy. Semaglutide acetate can be used in the study of type 2 diabetes.

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.